Pain removing compositions and methods

ABSTRACT

Pain removing compositions for external use on warm blooded animals. A pain removing composition is made from acetic acid, urea, ammonium hydroxide, glycerol, and water and may be used with plastiquinone A in a solvent. A binder may be used to tie the components together. A binder contains lanolin, stearic acid, water, triethanolamine and mineral oil. When rubbed on an external part of an affected area of a warm blooded animal, pain is removed in a short period of time.

United States Patent m: 3,

Gregory [451 Dec. 5, 1972 [541 PAIN REMOVING COMPOSITIONS [56] References Cited AND METHODS OTHER PUBLICATIONS [72] Inventor: Roy B. Gregory, 1130 N. 14th Street, Lafayette, 1nd. 47904 Chem- Abst 55 212766 1 Notice: The porgon of theDtermz g: Primary Examiner-Stanley J. Friedman patent sequent to 8 Attorney-Woodard, Weikart, Emhardt & Naughton has been disclaimed.

[22] Filed: Oct. 16, 1970 [57] ABSTRACT [21] Appl. No.: 81,555 Pain removing compositions for external use on warm Related Us. Application Data blooded animals. A pain removing composition is made from acetic acid, urea, ammonium hydroxide, [63] Continuation-in-part of Ser. No. 820,31 1, April glycerol, and water and may be used with plastiquin- 1969. one A in'a solvent. A binder may be used to tie the components together. A binder contains lanolin, stear- U.S- CI. ic acid water triethanolamine and mineral when 424/317 424/322, 424/332 rubbed on an external part of an affected area of a [51] Int. Cl. ..A6lk 27/00 warm blooded animal, pain is removed in a Short [58] Field of Search ..424/195, 332, 322, 168, 317, period of tin-la 4 Claims, No Drawings PAIN REMOVING COMPOSITIONS AND I METHODS CROSS REFERENCES TO RELATED APPLICATIONS This application is a continuation-in-part of applica- BACKGROUND OF THE INVENTION 1. Field of the Invention This invention is concerned with medicinal products of the pain remover type. More specifically this invention is concerned with external pain removers for use on warm blooded animals. The pain removers of this invention are particularly suited for use on humans.

2. Description of the Prior Art Pain removing compositions for external use are generally known in the prior art. Most of the prior art compositions contain ingredients which when applied to the surface of a warm blooded animal causes the area to feel hot or cold. These compositions generally change the flow rate of blood to the affected area. Common components in these prior art compositions are capsicum, chloroform, menthol, methyl salicylate, turpentine, camphor, oil of mustard, aspirin, narcotics, etc.

While the compositions and methods of the subject invention are similar to the above described prior ,art in that they are applied externally, their action is totally different because they do not draw more blood to the area in question or change the flow rate of blood in any manner.

Other prior art methods include massage, light rays, swirl baths, ultra sonic sound waves, etc. While these additional prior art methods bring some relief, they are disadvantageous in that they are time consuming and they are expensive.

Generally, it could be said that the prior art compositions and methods are slow to act and are only capable of rendering temporary relief. In contrast the present invention functions in a short period of time and it is capable of rendering relief which lasts for an extended period of time. It may be of interest to note that this invention also removes the pain and swelling due to injury or pain due to bursitis without any sensation that the pain and swelling is being removed.

SUMMARY OF THE INVENTION The invention is concerned with pain removing compositions for external use on warm blooded animals, methods of removing pain, and methods for the manufacture of the compositions. A pain removing composition is made from acetic acid, urea, ammonium hydroxide, glycerol and water. Plastiquinone A in a solvent may also be used in conjunction with the composition for prolonging the pain removing effect. A perfume can be added to cover the medicinal odor of the pain removing composition.

DESCRIPTION OF THE PREFERRED EMBODIMENT The pain remover of this invention is for external use on warm blooded animals. The compositions of this invention are specifically meant to be a pain remover and not a cure. This invention is for pain in muscle due to injury or contusions of external origin and pain in muscle caused by bursitis.

In contrast this invention is not for pain due to disease or pain due to internal disorder of vital parts of the body.

The subject composition generally has a composition in accordance with the percentages by volume as are specified in Table I.

TABLE I Acetic Acid 100%) 2.90 4% Urea (U.S.P.) 3.75 5% Ammonium Hydroxide (26%) 4.5 6% Glycerol (U.S.P.) 3 6| Water Balance A preferred composition in accordancewith this invention is set forth in Table II.

TABLE II Acetic Acid (100%) 3.33 Urea (U.S.P.) 4.18 Ammonium Hydroxide (26%) 5.00 Glycerol &U.S.P) 1 3.33 Water 84.16 100.00

The composition of this invention is generally prepared by diluting the acetic acid component with a small amount of water. To this diluted acetic acid is added the urea, which dissolves after shaking for a short period of time. The ammonium hydroxide is then added and then the glycerol. The glycerol disperses with vigorous agitation. The remainder of the water is added to produce a composite system. This composite system alone is effective in reducing pain.

It has been found that pain from some causes is only temporarily relieved with the composite system but may be permanently relieved with the additional use of plastiquinone A. The plastiquinone A may be produced by extracting finely divided fresh spinach chloroplast with a solvent for plastiquinone A for 12 hours. Heptane is the preferred solvent; however methanol, ethanol, acetone and petroleum ether are known solvents for plastiquinone A. Obviously the solvent chosen would have to be one which would not be harmful when applied externally.

The various solvents used would extract other compounds from the spinach but the other compounds would not be harmful or interfere with the pain reliever and may merely be left in the solvent. When heptane is used as a solvent with moist spinach leaves, a yield of 5 percent plastiquinone A by weight in the Heptane is obtained. is what is used in this invention. If the spinach is first freeze dried, the yield increases to 10 percent by weight. These spinach extracts work just as effectively as do similar percentages of pure plastiquinone A in pure heptane and are less expensive.

For best results the plastiquinone A is either applied I concurrently with or after application of the composite system are immiscible and thus must be vigorously shaken before use.

Binders may be added to slowdown or prevent the separation of the two immiscible mixtures. A binder for use in this invention is preferably prepared by mixing together at about 200F by volume about 16 percent lanolin, about 4 percent stearic acid, about 4 percent water and about 1 percent triethanolamine, upon cooling about 11 percent mineral oil is added along with sufficient water to make 100 percent.

The binder may be prepared by mixing together at about 180 to 212 F by volume about 14 to 18 percent lanolin, about 3 /2 to 5 percent stearic acid, about 3 to 6 percent water and about 1 to 2 percent triethanol amine, upon cooling 9 to 12 percent mineral oil is added along with sufficient water to make 100 percent.

Acceptable ranges of ingredients are by volume 5% plastiquinone A in heptane 3-90 percent, binder l-2O percent, and composite system 8-96 percent. Preferred percentages are by volume 5 percent plastiquinone A in heptane 4 percent, binder 2 percent, and composite system 94 percent.

When a binder is not used, mineral oil may be added to the heptane to prevent rapid drying on the surface of the skin. The amount used is not at all critical but generally about 3 percent mineral oil by volume is preferred. When a lanolin base hand or facial cream is added (about to 50 percent volume) to the plastiq uinone A in heptane a similar result is achieved.

The invention has a high concentration of each component in a small amount of solvent. This arrangement is advantageous because it does not allow each component to combine with other components completely, leaving some of each in a free or uncombined state. The free or uncombined molecules are necessary to react with the organic acids in the pain affected muscles to change these organic acids into products which the natural body metabolism can assimilate.

In addition to removing pain the subject composition is useful as a means of locating the exact point of injury. For example, when an entire arm and shoulder area hurts, a doctor cannot find the exact point of injury. Using this invention, a doctor can pin-point the exact point of injury in 45 minutes. The point of injury itself will remain tender to the touch. The doctor can then proceed with proper treatment to a speedy recovery. This is to be contrasted with the present methods employed by doctors which is to immobilize the arm and shoulder in a plaster cast and administer pain pills for relief. Sprains are immobilized and are soaked in hot packs or ice packs to reduce pain and swelling. The present invention makes these procedures unnecessary.

The composition of this invention functions by aiding in the rapid assimilation of the organic acids which are concentrated in the affected area and are responsible for the sensation of pain. I

Pain caused by injury is due mainly to a high concentration of oxalic, lactic and amino acids that radiate outward from point of injury. This invention will act on and react with these pain causing acids in the muscle changing these acids into non-harmful, non-painful products which the body metabolism can assimilate and move out very quickly. The oxalic and lactic acids are quickly changed by the subject composition into amines and are eliminated with this group.

Likewise, the composition of this invention causes an amino acid to inhibit the activity of one of the early enzymes in its pathwayflt quickly releases this inhibitor, restricts an oversupply of amino acids, unblocks their biosynthetic pathway and regulates their accumulation.

Finally, the subject composition increases protein synthesis allowing these acids to move out of affected area by natural body metabolism.

Injury due to accidents causes a build up of organic acids in muscles which slows down protein synthesis causing a surplus of the 19 other amino acids each of which shuts off its own biosynthetic pathway and thus contributes to a build up of intermediary catabolites which are corepressors of catabolic enzymes. Amino acids have the ability to inhibit the activity of one of the early enzymes in its biosynthetic pathway. Reduce the supply of amino acids by a factor or two, this reduction quickly releases this inhibition. Beginning 5 to 10 minutes after the shift down in amino acid supply, a marked depression of the enzyme con'cemed with the biosynthesis of the restricted amino acid occurs as a result of a reduced intracellular concentration of a repressing derivative of the amino acid. A near total repression of many catabolic enzymes begins within a few minutes of the amino acid shift down. The rapidity of response indicates this occurs independently of any long term affect of amino acid restriction such as reduced enzyme level. Protein synthesis and biosynthetic enzyme repression require the interaction of the'amino acid with the same specific aminoacyl synthetase.

This invention has the ability to reduce an amino acid supply, inhibit an enzyme, unblock their biosynthetic pathway, regulate their accumulation. increase protein synthesis cause these acids to be removed by natural body metabolism. Observation has shown that active acetate identified now as acetyl coenzyme A is involved in synthesis of fatty acids. Coenzyme A acts as a carrier not only for acetyl but for other acyl groups. The urea molecule reacts with these various acids with the help of ammonia and acetyl to change these acids into amines. The glycerol acts as a hydrogen and hydroxyl acceptor. Plastiquinone A activates coenzyme Q.

Coenzyme Q is located within the lipoprotein membrane of system of cells. Its activity is necessary for proper functioning of cells. Pain due to injury or irritation in muscle due to bursitis causes this enzyme to become dormant. The activity and function of coenzyme Q is necessary in the stringent cells to return these cells to normal structure and function. Plastiquinone A will activate coenzyme Q and keep it working. Plastiquinone A acts as an electron transport system .to transport energy through the cells farther away than next to or adjacent to each cell. There is a pool of quinone between the two sites to transfer energy from the site where electron flow occurs to the site where energy is used. Plastiquinone A undergoes rapid oridation and reduction during the electron transport process. Coenzyme Q undergoes rapid oxidation and reduction to account for the main unilateral electron transfer of protons and hydroxyl ions. As a result of this additional action pain and swelling does not return.

The following examples will illustrate the subject invention. These examples are given for the purpose of illustration and not for purposes of limiting this invention. The data for Examples 1 to 49 is listed in Table ill. in these examples the dosage was rubbed externally, on the affected area of the body. It can be seen from these examples that in a short period of time the pain in the affected area was removed and the relief lasted for an extended period. In the table under the Dosage column (formed from acetic acid, urea, ammonium hydroxide and glycerol). The letter O represents the use of 5 percent Plastiquinone A containing spinach extract with heptane as the solvent. The letter B indicates the use of a binder and the separates ingredients when a two solution form was used. m represents the use of mineral oil and 1 represents the use of a lanolin base the letter P represents the use of the composite system face cream.

TABLE III Time to Length Length of pain of time No. of Side time pain Name Example Pain due to- Age Dosage Sex removal present applns. etl'ects removed Comments .IW. 1 Bursitis 5O PQB M 30 min- 10 yrs. 1 None. 6 mos Could not raise nrm above shoulder-alter trvutimmt lrce movement-mo pain. GW- 2 .....do. 43 PQB M 40min 8 yrs.. 1 do. .1; mos Same. HR. 3 'lendonitis 66 P-l-Qm. M 45 min- 10 yrs... 30 ...do. 3 days to Intense pain broke sleep arm. 120 days. several times per nightrattlerf 2 treatments 90% pain re e PH. 4 Tcndonitis 56 P-l-Qm. M 15-35 min- 10 yrs... 5 ..do. 3 days, 5 Broke both feet and legs fell rheumatism. wks. 20 ft.has taken 3-4 pain pills per day for yrs. Alter 2 treatments 90% relief. BIL. 5 Rheumatism... 62 P+Qm. M 30 min- 12 yrs-.. 1 ...do. 6 mos Broken hip-auto accident has steel ball in socket. AH. 6 Tendonitis 58 P+Qm. M 45 min. 1 yr. 1 ..do. 4 mos Forearms, hands.

rheumatism. RB 7 Rheumatism 75 M 45 min.... 15 yrs... 1 ...do. 3 mos Shoulders. TM 8 Bursitis 40 3 ml. Pl M 40 min. 5 yrs.-.. 1 ame. HS.. 9 Bursitis 41 10 ml. Pl M 45min-..- 4yrs.... -1 ...do.-.. 6mos Same.

rheumatism V BL. 10 Bursitis 31 8ml. Pl M 45 min 1yr-.... 1 ...do. fimos Same. B11. 11 .....do 35 3ml. Pl M 45m1n.... 3yrs.... 1 ..-do.... Smos... Same. KR 12 .....do 25 3ml. P1.. M 45min-..- 2yrs.... 1 ..-do..-. fimos... Same. JS 13 Bursitis 62 6nd. P M 45min...- 8yrs.... 1 ...do.-.. 4mos Same.

rheumatism WB-.... 14 Bursitis 40 6 ml. M 45 min- 5 yrs.... 1 ...do. 3 mos Shoulders, arms and hands.

tendonitis. P+Qm. RN.-. 15 Tendonitis 48 3 ml. M 45 min- 8 yrs. 1 ...do. 6 mos Shoulder, forearm.

bursitis. P+Qm. DR... 16 Bursitis 38 3211M) M 45 min.... 5yrs.... 1 do--.- 1hr Shoulder.

m. RH... 17 .....do 37 m1. M 45 min.... 5yrs.... 1 ...do.... 10 mos Same. y, P+Qm. 08...... 18 .....do........... 40 1-3 ml. M 45 min.. 3 yrs-... 1 ...do..... 6 mos Same.

P-i-Qm. LL..... 1) ..d0....... 40 1-3 ml. M 45 min. 2yes 1 ..-do 6mos Same.

P-l-Qm. JR 20 .d 38 1-8 ml. M 40 min.-.- 3yrs.-.. 1 ..-do..... 8mos..' Same. P+Qm. RK... 21 Rheumatism... 45 1-5 ma M 35 min..-. yrs.- 1 ...do.. 1 yr Same.

P+ in. RI)... 2.! Bursitis... 38 1-3 mg M 45 min.. 3 yrs.-..' 1 ...do..... 6 mos Same.

PQ CR. 23 Bursitis 52 1 5 ml. M 45 min.... yrs... 1 ..-do...-. 8 mos Same.

rheumatism. PQB R'l. 24 Tondonitis 55 15 ml. M 45 min...- 5 yrs.- 2 ...do..... 2-6 mos-.- Legs and heel. rheumatism. PQB RS..... 25 Rhcumatism. 45 15 I6]. M 30 min..-. 3 yrs.- 1 ...do..... 6 mos Shoulder.

P B. RB. 26 Tendonitis 58 1-3 ml. M -30 minyrs.-. 10 .-do..... 1-3 mos..-.. Shouder, arms.

bursitis PQB. 11R... 27 Jammed 63 10 ml. P-.. F 40 min..-. 2 /5 mos- 1 .-.do..... Did not Doctor treated 30 days shoulder. return Osteopath treated 2 times 1 yr. per week for 5 weeks, no result-1 treatment pain gone- MS.... 28 Sprained finger.- 78 ml. F min. 2 wks-.- 1 ..do........ ..do...... Doctor X-rayed. Finger stifi, P+Q1 could not use-1 treatment complete movement, no p n. MF- 29 sprained elbow. 58 15 ml. 25 min.-.- 10 yrs... 1 ...do... ......do....-.. Fell from house. Pain daily P+Q1 1 treatment pain removed. DF. 30 Arthritis 61 1{nil Q1 F 40 min. 2 yrs.- 1 ..-do..... 8 mos Hands. MD... 31 Rheumatism 19 ml. F 20 min..-. 3 yrs.... 1 ..-do..... 5 mos Has taken 2 aspirin 6 times a shoulders. P+Ql day, shoulder point of injury right clavicle. l)S..... 32 Arthritis 48 142 23.21 F 45 min.-.- 5 yrs-... 3 ..-do..-.. 1-4 mos-.. Elbow and hands. M 33 .....(l0........... 43 Hligmlil F 45 min..-. 4yrs.... 2 ...do..... 1-6 mos-.- Shoulders.

'i' MS..... 34 Rheumatism.... 48 kg rinLl F 45 min.... 2 yrs.... 1 ...do.... 4 mos Upper back.

Q MD. 35 Sprained ankle.- 41 1-5 ml. F 45 min. 1 wk.... 1 ...do.... Did not Pain and swelling removed.

P+Qm. I return 1 year. 36 Rheumat1sm... 62 3-6 ml. P.. F 30 min.-.. 2 yrs..-. 1 -..do.. 6 mos Legs (pain removed). 37 .....do 57 3-6ml. P.. F 30 min.... 7 yrs---. 1 ...do..... ,6 mos-.. Shoulders. 38 .....do 65 3-6 ml. P.. F 45 11111-... 10 yrs..- -3 ...do..... 14mos..... Legs. 30 J emmed 40 8-10 ml. F min.... 3 mos... 1 do... Did not Has taken physiotherapy. shoulder. P. return 1 Injury 4th-5th vertebra.

1 year 111'. 40 Sprained wrist 52 1-3 ml. P.. F 45 min. 1 wk.... 1 -..do ..do Swelling and pain removed. GL..... 41 sprained ankle. 57 10 m1. F 45 min- 2 days- 1 --.do..... Did not Same.

' return. J'I 43 sprained wrist. 43 '3ml. P. F 30 min.... 2wks... 1 ...do ..do Pain removed. MS. 43 Arthritis 1 10 ml. F 45 min-... 5 yrs. 1 ..do..... 10 mos Arms, legs.

rheumatism. PBQ. LN. 44 Rheumatismm. 51 10 ml F 45 min.... 5 yrs.... 1 -..do..... 10 mos Upper back.

'l'uhlc Ill-Continued I Time to Length Length of pain of time No. of Side time pain Namt hxamplr: Pain due to-- Age Dosage Sex removal present applns. effects removed Comments AG 45 ..-do 60 lo g F 45112111.... 10 yrs... 1 ...do..... rnos Hips and legs. L1... 46 Rheumatism 57 8-10 ml F 40 min.. yrs... 1 ---do....- 2-4 mos Upper back and arms.

arthritis. PQB. Nil 47 Rheumatism.. 30 P F 30 min.... 1yr 1 ..do Gmos Lower back. RH. 48 lnjured 76 P+Q1. M 35 min.... yrs... 1 -do..- 6 mos Had been takingnltra sonic shoulder, sounlg treatments with no resu s. AH. 4E) Pulled tendon. 41 P-l-Q. M 35min...- 2 yrs.... 3 ...do....- 6 mos Pain removed.

1 pm day.

What is claimed is:

1. A process for the manufacture of a pain removing composition which comprises with percentage by volume diluting from 2.9 to 4 percent of acetic acid with a small amount of water to allow ionization, adding to the acetic acid from 3.75 to 5 percent of urea, after the urea has dissolved, adding from 4.5 to 6 percent of 26 percent ammonium hydroxide, to the dissolved urea, then adding from 3 to 6 percent of glycerol and adding water to make 100 percent.

2. A pain removing composition as is produced by the method of claim 1.

3. A process for making a pain removing composition comprising making a binder by mixing together at about l to 212 F by volume 14 to 18 percent lanolin, about 3't0 6 percent water and about 1 to 2 percent triethanol amine, upon cooling 9 to 12 percent mineral oil is added along with sufficient water to make 100 percent, mixing 1 to 20 percent of this binder with 3 to percent of 5 percent plastiquinone A in heptane and with 8 to 96 percent of the composition produced by the method of claim 1.

4. A method for treating pain which comprises external application to a patient of the composition produced by the process of claim 1. 

2. A pain removing composition as is produced by the method of claim
 1. 3. A process for making a pain removing composition comprising making a binder by mixing together at about 180* to 212* F by volume 14 to 18 percent lanolin, about 3 to 6 percent water and about 1 to 2 percent triethanol amine, upon cooling 9 to 12 percent mineral oil is added along with sufficient water to make 100 percent, mixing 1 to 20 percent of this binder with 3 to 90 peRcent of 5 percent plastiquinone A in heptane and with 8 to 96 percent of the composition produced by the method of claim
 1. 4. A method for treating pain which comprises external application to a patient of the composition produced by the process of claim
 1. 